Synthesis, characterization and investigation of AChE and BuChE inhibitory activity of 1-alkyl-4-[(5,6-dimethoxy-1-indanone-2-yl)methylene]pyridinium halide derivatives
Sign Up to like & getrecommendations! Published in 2019 at "Journal of the Iranian Chemical Society"
DOI: 10.1007/s13738-019-01804-1
Abstract: Abstract The design, synthesis and characterization of a series of 1-alkyl-4-[(5,6-dimethoxy-1-indanone-2-yl)methylene]pyridinium halide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors for the treatment of Alzheimer’s disease were reported. The strategy for this synthesis was based on aldol… read more here.
Keywords: alkyl dimethoxy; buche; dimethoxy indanone; methylene ... See more keywords
Synthesis, molecular docking and molecular dynamics studies of novel tacrine-carbamate derivatives as potent cholinesterase inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2021.105225
Abstract: In the present study, new tacrine derivatives containing carbamate group were synthesized and their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition activities were evaluated. All synthesized compounds inhibited both cholinesterases at nanomolar level. Among them, ((1,2,3,4-tetrahydroacridin-9-yl)amino)ethyl(3-nitrophenyl)… read more here.
Keywords: synthesized compounds; buche; carbamate derivatives; carbamate ... See more keywords
In silico modeling for dual inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes in Alzheimer's disease
Sign Up to like & getrecommendations! Published in 2020 at "Computational biology and chemistry"
DOI: 10.1016/j.compbiolchem.2020.107355
Abstract: In this research, we have implemented two-dimensional quantitative structure-activity relationship (2D-QSAR) modeling using two different datasets, namely, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzyme inhibitors. A third dataset has been derived based on their selectivity and… read more here.
Keywords: acetylcholinesterase ache; buche; inhibition; number ... See more keywords
Tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one scaffold derivatives: Synthesis and biological evaluation as selective BuChE inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.02.002
Abstract: BuChE inhibitors play important roles in treatment of patients with advanced Alzheimer's disease (AD). A series of tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one derivatives were synthesized and evaluated as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors. Some derivatives showed selective… read more here.
Keywords: tricyclic pyrazolo; buche inhibitors; selective buche; buche ... See more keywords
Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT6R antagonists with β-amyloid anti-aggregation properties.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113792
Abstract: The lack of an effective treatment makes Alzheimer's disease a serious healthcare problem and a challenge for medicinal chemists. Herein we report interdisciplinary research on novel multifunctional ligands targeting proteins and processes involved in the… read more here.
Keywords: aggregation; buche; crystallography aided; development crystallography ... See more keywords
A Simple 3D-printed Enzyme Reactor Paper Spray (3D ER-PS) Mass Spectrometry Platform for Detecting BuChE Activity in Human Serum.
Sign Up to like & getrecommendations! Published in 2019 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.9b02728
Abstract: To achieve personalized healthcare, a quick, accurate and high-throughput method to detect disease biomarkers is essential. In the traditional practice, mass spectrometry is one of the most powerful tools and is widely studied. However, the… read more here.
Keywords: mass spectrometry; buche; paper; human serum ... See more keywords
Discovery of New 1,3,4-Oxadiazoles with Dual Activity Targeting the Cholinergic Pathway as Effective Anti-Alzheimer Agents.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.1c00766
Abstract: Finding an effective anti-Alzheimer agent is quite challenging due to its multifactorial nature. As such, multitarget directed ligands (MTDLs) could be a promising paradigm for finding potential therapeutically effective new small-molecule bioactive agents against Alzheimer's… read more here.
Keywords: ache buche; buche; anti alzheimer; effective anti ... See more keywords
A patent review of butyrylcholinesterase inhibitors and reactivators 2010–2017
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DOI: 10.1080/13543776.2018.1476494
Abstract: ABSTRACT Introduction: Butyrylcholinesterase (BuChE) has obtained a renewed interest as therapeutic target in Alzheimer’s disease (AD), when changes in BuChE activity and expression along disease progression were highlighted as well as correlation between BuChE levels… read more here.
Keywords: patent review; butyrylcholinesterase; buche inhibitors; buche ... See more keywords
Aaptamine – a dual acetyl – and butyrylcholinesterase inhibitor as potential anti-Alzheimer’s disease agent
Sign Up to like & getrecommendations! Published in 2022 at "Pharmaceutical Biology"
DOI: 10.1080/13880209.2022.2102657
Abstract: Abstract Context Alzheimer’s disease (AD) is a neurodegenerative disorder that affects millions of people worldwide. Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) are promising therapeutic targets for AD. Objective To evaluate the inhibitory effects of aaptamine on… read more here.
Keywords: alzheimer disease; buche; anti; ache buche ... See more keywords
A hybrid of 1-deoxynojirimycin and benzotriazole induces preferential inhibition of butyrylcholinesterase (BuChE) over acetylcholinesterase (AChE)
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2117912
Abstract: Abstract The synthesis of four heterodimers in which the copper(I)-catalysed azide-alkyne cycloaddition was employed to connect a 1-deoxynojirimycin moiety with a benzotriazole scaffold is reported. The heterodimers were investigated as inhibitors against acetylcholinesterase (AChE) and… read more here.
Keywords: acetylcholinesterase ache; buche; benzotriazole; preferential inhibition ... See more keywords
Relationship Between Paraoxonase-1 and Butyrylcholinesterase Activities and Nutritional Status in Mexican Children.
Sign Up to like & getrecommendations! Published in 2018 at "Metabolic syndrome and related disorders"
DOI: 10.1089/met.2017.0138
Abstract: BACKGROUND The enzymes butyrylcholinesterase (BuChE) and paraoxonase-1 (PON1) are the primary bioscavenging enzymes in serum and exhibit antioxidant and anti-inflammatory activities. PON1 has been associated with diseases caused by high oxidative stress, whereas BuChE appears… read more here.
Keywords: pon1 l55m; buche; pon1; nutritional status ... See more keywords